Cancer is the leading cause of mortality worldwide. In patients with metastatic non-small cell lung cancer, epidermal growth factor receptor (EGFR) is often overexpressed. Gefitinib (GEF), an inhibitor of EGFR, is approved for the treatment of patients with metastatic non-small cell lung cancer (NSCLC). However, the low solubility and dissolution of GEF limits its bioavailability. Numerous methods, including solid dispersion (SD) and complexation, have been reported to enhance the dissolution of poorly soluble drugs. In this study, GEF complexes were prepared using methyl-β-cyclodextrin (MβCD) and hydroxypropyl-β-cyclodextrin (HPβCD) in two molar ratios (1:1 and 1:2), furthermore, GEF SDs were prepared using polyvinylpyrrolidone (PVP), polyethylene glycol (PEG), and poloxamer-188(PXM) in three different ratios (1:2, 1:4 and 1:6 w/w). Dissolution studies were conducted on the prepared formulations. Dissolution results showed a 1.22-2.17-fold enhancement in drug dissolution after one hour compared to untreated GEF. Two formulations that showed higher dissolution enhancement were subsequently evaluated for in-vitro cytotoxicity and were formulated into tablets. The selected PVP-GEF (1:4 w/w) and MβCD-GEF (1:1M) formulas displayed improved cytotoxicity compared to untreated GEF. The IC values of the PVP-GEF and MβCD-GEF were 4.33 ± 0.66 and 4.84 ± 0.38 µM, respectively which are significantly lower (p < 0.05) than free GEF. In addition, the formulated tablets exhibited enhanced dissolution compared to pure GEF tablets. PVP-GEF SD tablets released (35.1 %.4) of GEF after one hour, while GEF-MβCD tablets released (42.2 % after one hour. In the meantime, tablets containing pure GEF showed only 15 % 0.5 release at the same time. The findings of this study offer valuable insights for optimizing the dissolution and hence therapeutic capabilities of GEF while mitigating its limitations.
Download full-text PDF |
Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC11031755 | PMC |
| http://dx.doi.org/10.1016/j.jsps.2024.102070 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Phosphorus-solubilizing fungi promote the growth of P. Y. Li by regulating physiological and biochemical reactions and protecting enzyme system-related gene expression.
Front Genet
January 2025
Chongqing Engineering Laboratory of Green Planting and Deep Processing of Famous-Region Drug in the Three Gorges Reservoir Region, College of Biology and Food Engineering, Chongqing Three Gorges University, Chongqing, China.
Introduction: P. Y. Li is a plant used to treat respiratory diseases such as pneumonia, bronchitis, and influenza.
View Article and Find Full Text PDFEnvironmentally Friendly and Simple Recycling of Titanium Alloy Scrap via Deoxygenation with Hybrid Hydrogen Plasma Arc.
Adv Sci (Weinh)
January 2025
School of Materials Science and Engineering, Harbin Institute of Technology, Harbin, 150001, China.
The potential of hydrogen plasma arc technology for the efficient deoxygenation and recycling of titanium alloy scrap is explored. The results of thermodynamic analysis reveal that hydrogen plasma is suitable for oxygen removal. The intermediate stages of the deoxygenation process are sequentially analyzed, showing that the hydrogen plasma arc primarily facilitated the reduction and dissolution of oxides as well as eliminated interstitial oxygen.
View Article and Find Full Text PDFStatus analysis of quality control of administered infusion solution with cytotoxic drugs.
Oncol Rev
January 2025
Department of Pharmacy, Tianjin First Central Hospital, Nankai University, Tianjin, China.
The administered infusion solution is a sterile preparation that can be used directly for intravenous infusion in patients by mixing one or more intravenous drugs using aseptic operation technology. The pharmacy intravenous admixture service (PIVAS) center is a professional technical service department in hospitals, where the majority of inpatient-administered infusion solutions are prepared. During the processes of dissolution, dilution, preparation, storage, and use of intravenous drugs, the quality control of the administered infusion solution can be affected by various factors.
View Article and Find Full Text PDFAssessment on surface integrity in electrochemical grinding of AISI 304.
Heliyon
January 2025
Advanced Technologies of Machine Tools (ATMT) Lab, Faculty of Mechanical Engineering, Tarbiat Modares University, Tehran, Iran.
Electrochemical grinding (ECG) offers advantages such as burr-free and stress-free material removal. Despite its proven potential, limited research has addressed the comprehensive effects of key process parameters on the surface integrity of AISI 304 stainless steel, particularly for applications requiring high-quality finishes, such as medical components. This study bridges this gap by systematically investigating the influence of ECG key parameters including voltage, rotational speed, and electrolyte concentration on main surface integrity parameters including current density, surface roughness, microhardness, and surface texture.
View Article and Find Full Text PDFLithium recovery from mixed spent LFP-NMC batteries through atmospheric water leaching.
Sci Rep
January 2025
Technology Innovation, PT Pertamina (Persero), Jl. Raya Bekasi KM. 20 Cakung, East Jakarta, Jakarta, 13920, Republic of Indonesia.
Selective lithium recovery from a mixture of LFP-NMC spent lithium batteries presents significant challenges due to differing structures and elemental compositions of the batteries. These differences necessitate a distinct recycling pathway for each, complicating the process for the mixture. This study explored a carbothermal reduction approach combined with water leaching under atmospheric conditions to achieve a selective lithium recovery.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!